Chalcogen Bonded Directly To The Bicyclo-carbocyclic Ring System Patents (Class 546/206)
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Patent number: 5489599Type: GrantFiled: June 28, 1993Date of Patent: February 6, 1996Assignee: Shell Research LimitedInventors: Paul A. Carter, Steven J. Tapp, Nicholas J. Daniels
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Patent number: 5472966Abstract: Certain aminoalkyl derivatives of naphthyl-piperidines and tetrahydro-pyridines of Formula (I) are useful antidepressant agents. ##STR1## The symbol (Aryl) denotes phenyl, naphthyl, pyridinyl, pyrimidinyl and pyrazinyl ring systems with n being an integer of 2-4.Type: GrantFiled: March 29, 1995Date of Patent: December 5, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Charles P. Sloan, David W. Smith
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Patent number: 5461045Abstract: A fused benzeneoxyacetic acid derivative of the formula: ##STR1## wherein ##STR2## is (i) ##STR3## (ii) ##STR4## (iii) ##STR5## or (iv) ##STR6## A is (i) ##STR7## or (ii) ##STR8## R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl or phenyl;R.sup.3 is(i) C.sub.1-15 alkyl,(ii) C.sub.1-8 alkyl substituted by one or two of benzene, C.sub.4-7 cycloalkane or 4-7 ring-membered monocyclic ring which contains one nitrogen atom or(iii) C.sub.10-15 condensed tricyclic ring;e is 3-5;f is 1-3;p is 0-4;q is 0-2;s is 0-3With the proviso that, ring(s) in R.sup.3 may be substituted by one to three of C.sub.1-4 alkyl, .sub.1-4 alkoxy, halogen atom, nitro or trihalomethyl. And, when D--B is the formula (iii) or (iv), --(CH2)p- or .dbd.CH--(CH2)s- is attached at the position of a or b on the ring.Type: GrantFiled: July 14, 1992Date of Patent: October 24, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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Patent number: 5457207Abstract: The compounds are vesamicol (hydroxylated phencyclidine (PCP) isomer trans-2-(4-phenyl-piperidino)cyclohexanol) derivatives with anticholinergic properties termed herein "spirovesamicols" which are spirofused piperidines. The compounds bind to the vesamicol receptor, a site on the cholinergic synaptic vesicle, which is associated with the vesicular transporter of acetylcholine.Type: GrantFiled: October 5, 1993Date of Patent: October 10, 1995Assignee: Regents of the University of MinnesotaInventors: Simon M. N. Efange, Stanley M. Parsons
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Patent number: 5446052Abstract: The invention relates to aromatic amino derivatives of formula ##STR1## wherein, R, T, Z, Ar', T', Z' are defined in the specification and their enantiomers, processes for their production and their use for the treatment of substance p- and neurokinin-dependent pathology.Type: GrantFiled: February 4, 1994Date of Patent: August 29, 1995Assignee: SanofiInventors: Xavier Emonds-Alt, Isabelle Grossriether, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5436343Abstract: Compounds of formula (I): ##STR1## in which: R.sub.1 and R.sub.2, which may be identical or different, represent a linear or branched (C.sub.1 C.sub.6) alkyl radical, a substituted or unsubstituted phenyl radical, a pyridyl radical or a thienyl radical, or, with the carbon atom to which they are attached, a substituted or unsubstituted (C.sub.4 -C.sub.7) cycloalkyl ring,R.sub.3 representsa substituted or unsubstituted phenylsulfonyl radical,a linear or branched (C.sub.1 -C.sub.6) alkyl radical,an alkylaminocarbonyl radical,or a linear or branched (C.sub.1 -C.sub.6) acyl radical,R.sub.4 represents any one of the radicals:--CH.dbd.CH--(CH.sub.2).sub.p --CO.sub.2 H or --CH.sub.2 --CH.sub.2 --(CH.sub.2)p--CO.sub.2 Hin which p is equal to 0, 1, 2 or 3, n and m, which may be identical or different, represent 0, 1 or 2,their isomers, enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid or base.Type: GrantFiled: May 14, 1993Date of Patent: July 25, 1995Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Michel Laubie, Tony Verbeuren
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Patent number: 5428042Type: GrantFiled: December 23, 1992Date of Patent: June 27, 1995Assignee: Dr Lo Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Roberto Colle, Giuseppe Giardina
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Patent number: 5410046Abstract: Synthetic intermediates of 1-arylethyl-3-substituted piperidines.Type: GrantFiled: May 11, 1993Date of Patent: April 25, 1995Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross, Robert M. Wallis
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Patent number: 5382687Abstract: An enamine derivative containing a fluoroalkyl group, a fluoroaryl group or a fluoroaralkyl group is effective as a charge transport material in an electrophotographic member excellent in sensitivity, residual potential, durability and the like electrophotographic properties.Type: GrantFiled: August 2, 1993Date of Patent: January 17, 1995Assignee: Hitachi Chemical Company Ltd.Inventors: Yoshii Morishita, Shigeru Hayashida, Yasushi Sugimoto, Hiroko Ishikawa, Hiroshi Kobayashi, Takaaki Sonoda
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Patent number: 5366981Abstract: A compound, a solvate or salt thereof, of formula (I): ##STR1## in which: A is ##STR2## p is 2; ROC-- is an acyl group linked to a substituted or unsubstituted carbocyclic aromatic ring system;R.sub.1 and R.sub.2 are substituents on the same or different carbon atoms and are independently hydrogen or C.sub.1-6 alkyl; andR.sub.a is a phenyl or thienyl ring, andis useful for the treatment of pain, hyponatremic disease states or cerebral ischemia.Type: GrantFiled: May 22, 1992Date of Patent: November 22, 1994Assignee: Dr Lo Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Roberto Colle, Giulio Dondio, Giuseppe Giardina
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Patent number: 5356905Abstract: 3-Piperidino-1-chromanol derivatives and analogs having the formula ##STR1## wherein A and B are taken together and are --CH.sub.2 CH.sub.2 -- or A and B are taken separately and are each H;X is CH.sub.2 or O;X.sup.1 is H or OH;Z is H, F, Cl, Br or OH;Z.sup.1 is H, F, Cl, Br or (C.sub.1 -C.sub.3)alkyl;n is 0 or 1; andm is 0 or an integer from 1 to 6;pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.Type: GrantFiled: July 23, 1992Date of Patent: October 18, 1994Assignee: Pfizer Inc.Inventor: Todd W. Butler
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Patent number: 5354904Abstract: The sulfonamides have the formula ##STR1## where R.sup.1 is C.sub.1 -C.sub.13 -lkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.8 -alkanoyl or substituted or unsubstituted benzoyl, andR.sup.2 and R.sup.3 are each independently of one another substituted or unsubstituted C.sub.1 -C.sub.13 -alkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkyl or substituted or unsubstituted piperidinyt, or R.sup.2 may also be hydrogen.Type: GrantFiled: October 8, 1992Date of Patent: October 11, 1994Assignee: BASF AktiengesellschaftInventors: Udo Mayer, Ulrike Schloesser
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Patent number: 5344835Abstract: According to the invention there is provided a compound of formula (I): R.sup.1 --O(CH.sub.2).sub.m A(CH.sub.2).sub.n XR or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is a group of formula (a or b) where Z is --(CH.sub.2).sub.2-, --CH.dbd.CH--, --CH.sub.2 --S-- or --CH.sub.2 --O--; R is a group of formula (c, d or Het) and A is a group of formula (e, f or g) in which the N atom is attached to the group (CH.sub.2)n; m is 1 or 2; n is an integer of from 1 to 4; p is 1, 2 or 3; R.sup.2 and R.sup.3 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy-(C.sub.1 -C.sub.4 alkyl), hydroxy, C.sub.1 -C.sub.4 alkoxy, halo, trifluoromethyl, nitro, cyano, sulphamoyl, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), carboxy, --CO.sub.2 (C.sub.1 -C.sub.4 alkyl), --CH.sub.2).sub.q CONR.sup.4 R.sup.5, -- (CH.sub.2).sub.q OCONR.sup.4 R.sup.5, --CH.sub.2).sub.q NR.sup.6 R.sup.7 or --NHSO.sub.2 NH.sub.2 in which R.sup.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.Type: GrantFiled: July 2, 1992Date of Patent: September 6, 1994Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross
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Patent number: 5328917Abstract: The present invention relates to piperidine derivatives of the formula: ##STR1## wherein, R, R.sup.1, R.sup.3, X, and n are defined in the specification, pharmaceutical compositions thereof and methods of treating anoxia, traumatic injury, ischemia, migraine and epilepsy.Type: GrantFiled: May 20, 1993Date of Patent: July 12, 1994Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Anders Kanstrup, Jane M. Lundbeck
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Patent number: 5326771Abstract: Piperidylmethyl-substituted chroman derivatives can be prepared by first reducing corresponding chromancarboxylic acid derivatives, if appropriate with prior activation, with the cyclic amines and then reducing the carbonyl group, or by reacting chromanmethyl compounds directly with the cyclic amines. The substituted piperidylmethyl-substituted chroman derivatives can be employed as active compounds in medicaments, in particular for the treatment of diseases of the central-nervous system.Type: GrantFiled: November 30, 1992Date of Patent: July 5, 1994Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Heine, Bodo Junge, Peter-Rudolf Seidel, Rudolf Schohe-Loop, Thomas Glaser, Jean M. V. De Vry, Wolfgang Dompert, Henning Sommermeyer
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Patent number: 5318994Abstract: Compounds of the formula: ##STR1## in which: A represents ##STR2## R represents linear or branched lower alkyl, R.sub.1 represents hydrogen or linear or branched lower alkyl, andR.sub.2 represents aryl or lower arylalkyl or aryl or lower arylalkyl substituted by lower alkyl, lower alkoxy, trifluoromethyl, or halogen, aryl means phenyl or naphthyl, as well as optical isomers, epimers and diastereoisomers and addition salts thereof with a pharmaceutically-acceptable acid, lower alkyl and lower alkoxy having 1 to 6 carbon atoms inclusive, andmedicaments containing the same which are useful for the treatment of disorders of the melatoninergic system.Type: GrantFiled: November 3, 1992Date of Patent: June 7, 1994Assignee: Adir et CompagnieInventors: Jean Andrieux, Raymond Houssin, Said Yous, Beatrice Guardiola, Daniel Lesieur
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Patent number: 5306720Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from substituted or unsubstituted quinazolinedione,X denotes a group of the formula ##STR2## n is an integer of 1 through 7, the ring A denotes a group of the formula ##STR3## a group of the formula ##STR4## or a group of the formula ##STR5## and R.sup.2 denotes a hydrogen atom, a lower alkyl group, a substituted benzoyl group, a pyridyl group, a 2-hydroxyethyl group, a pyridylmethyl group, or a group of the formula ##STR6## wherein Z represents a halogen atom). The novel compounds of this invention are used for treating dementias and sequelae of cerebrovascular diseases.Type: GrantFiled: December 20, 1991Date of Patent: April 26, 1994Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 5298513Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine ora group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andX denotes oxygen, sulphur or NR.sup.5,and their salts.Type: GrantFiled: May 29, 1992Date of Patent: March 29, 1994Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 5281720Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: October 26, 1992Date of Patent: January 25, 1994Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Yves Girard, John W. Gillard, Laird A. Trimble, John Scheigetz, James A. Yergey, Yves Ducharme, Deborah A. Nicoll-Griffith, John H. Hutchinson
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Patent number: 5272144Abstract: Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula ##STR1## wherein each of A and B is a group of formula (i) to (iii): ##STR2## wherein Y is --O--, --S-- or --NR-- in which R is hydrogen or C.sub.1 -C.sub.6 alkyl; each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is independently:a) hydrogen, halogen, hydroxy, cyano or nitro;b) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen,c) C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;d) C.sub.1 -C.sub.6 alkyl-sulfonyl;e) a substituted amine group --NR.sub.7 R.sub.8 ;f) a --COR.sub.12 group; org) two adjacent groups of R.sub.3, R.sub.4, R.sub.5 and R.sub.6, taken together, form a C.sub.1 -C.sub.4 alkylenedioxy group;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkenyl or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl; or R.sub.1 and R.sub.Type: GrantFiled: June 13, 1991Date of Patent: December 21, 1993Assignee: Farmitalia Carlo Erba s.r.l.Inventors: Piero Melloni, Philippe Dostert, Arturo D. Torre, Alberto Bonsignori
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Patent number: 5272157Abstract: Compounds of general formula (I) ##STR1## in which n is 1 or 2;R represents a linear or branched C.sub.1 -C.sub.3 -alkyl group; andX represents at least one substituent chosen from hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl and C.sub.1 -C.sub.3 -alkoxy, in the form of a free base or an acid addition salt thereof, and their therapeutic application.Type: GrantFiled: November 17, 1992Date of Patent: December 21, 1993Assignee: SynthelaboInventors: Pascal George, Jacques Froissant, Mireille Sevrin
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Patent number: 5270327Abstract: Analgesic compounds of the formula (I): ##STR1## in which, R.sup.1 R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a 5-6-membered N-heterocyclic ring optionally having a further O, N, or S heteroatom; E represents methylene; ring A is an unsubstituted or substituted benzene or naphthalene; R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(=Y)-- (IV)wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen with up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygens.Type: GrantFiled: September 10, 1992Date of Patent: December 14, 1993Assignee: Sankyo Company, LimitedInventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
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Patent number: 5252589Abstract: There is disclosed a benzocycloheptene compound of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, a halogen atom or a lower alkoxy group, R.sup.2 and R.sup.3 are independently selected from hydrogen atom, a lower alkyl group and a lower alkenyl group, or R.sup.2 and R.sup.3 combine together with adjacent nitrogen atom to form a heteromonocyclic group, or a pharmaceutically acceptable salt thereof, which has an excellent inhibitory activity against contraction of urinary bladder.Type: GrantFiled: December 14, 1992Date of Patent: October 12, 1993Assignee: Tanabe Seikayu Co., Ltd.Inventors: Masakatsu Ozeki, Kosuke Yasuda, Masamichi Morimoto, Tohru Ishizuka, Kunio Nosaka
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Patent number: 5250550Abstract: There are disclosed novel complexes of nitric oxide and polyamines which are useful in treating cardiovascular disorders, including hypertension. The disclosed compounds release nitric oxide (endothelium-derived relaxing factor) under physiological conditions in a sustained and controllable fashion, and possess long mechanisms of action.Type: GrantFiled: June 30, 1992Date of Patent: October 5, 1993Assignee: The Government of the United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Larry K. Keefer, Joseph A. Hrabie
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Patent number: 5250544Abstract: The invention relates to compounds of formula I: ##STR1## in which R.sub.1 represents a naphthyl radical, a dihydronaphthyl radical, a tetrahydronaphthyl radical, a quinolyl radical or a 1,4-benzodioxanyl radical, A represents a single bond, a double bond, a methylene radical, a radical of formula z.sub.1 :--CH.dbd. (z.sub.1)or a radical of formula z.sub.2 :.dbd.CH-- (z.sub.2)the ring B represents a piperidyl radical, a pyrrolidinyl radical, or a 1,2,3,6-tetrahydropyridyl radical, and R.sub.2 represents: a hydrogen atom, a benzyl radical, or an alkyl radical having 1 to 6 carbon atoms, on condition that in one of these cases R.sub.1 is other than a naphthyl (y.sub.1), dihydronaphthyl (y.sub.2) or tetrahydronaphthyl (y.sub.3) radical and B is other than a piperidinyl radical, or an aminoalkyl radical having 1 to 6 carbon atoms, a cyanoalkyl radical having 1 to 6 carbon atoms, or a radical of formula w.sub.1 : ##STR2## in which n is 1-6 and R.sub.Type: GrantFiled: July 1, 1991Date of Patent: October 5, 1993Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Michel Laubie, Francis Colpaert
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Patent number: 5248673Abstract: The present invention provides new thrombin inhibiting bisamidines derivatives, their pharmaceutically acceptable salts and hydrates, methods for their preparation, pharmaceutical composition, a process for their preparation, and use of the compounds in treatment of thrombosis, ischemia and stroke.Type: GrantFiled: December 23, 1992Date of Patent: September 28, 1993Assignee: Bristol-Myers Squibb Co.Inventors: Neelakantan Balasubramanian, William T. Han
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Patent number: 5245034Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: March 23, 1992Date of Patent: September 14, 1993Assignee: Kiroyoshi HidakaInventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5234933Abstract: Novel cyclic hydroxamic acids of the general formula: ##STR1## wherein ring A is 5- or 6-membered; R.sup.1, R.sup.2 and R.sup.3 each, ipendently, is hydrogen, C1-24 alkyl, C2-24 alkenyl or a group of the formula: ##STR2## wherein R.sup.4, R.sup.5, R.sup.7 and R.sup.8 each, independently is hydrogen,C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, halogen or nitro; l is 1-3; m is 1-3; n is 1-3; k is 1-3;R.sup.6 and R.sup.9 each, independently is C1-24 alkylene or C2-24 alkenylene;With the proviso that, more than one of R.sup.1, R.sup.2 and R.sup.3 are not hydrogen at the same time; and the pharmaceutically acceptable salts thereof possesses an inhibitory activity against 12-lipoxygenase, and therefore, may be useful for treating and/or preventing inflammation, immune diseases, psoriasis, arteriosclerosis and/or ischaemic cardiovascular diseases and also for suppressing metastasis of cancer.Type: GrantFiled: October 31, 1991Date of Patent: August 10, 1993Assignee: Board of Governors of Wayne State University and Vanderbilt UniversityInventors: Lawrence J. Marnett, Kenneth V. Honn, Carl R. Johnson, Yung-fa Chen, Katsu-ichi Shimoji
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Patent number: 5216150Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: September 12, 1991Date of Patent: June 1, 1993Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5214141Abstract: The present invention relates to an azomethine compound represented by formula (I): ##STR1## wherein X represents a 5- or 6-membered cyclic amino group, R represents an aromatic group, and Ar represents an aromatic group having an aliphatic amino group in the para-position. The azomethine compounds disclosed are useful yellow dyes for photography, for various optical filters, for ink jet, for heat transfer printing, and for printing.Type: GrantFiled: December 31, 1991Date of Patent: May 25, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Masuji Motoki, Naoki Saito, Takayoshi Kamio, Mitsugu Tanaka, Seiji Ichijima
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Patent number: 5212182Abstract: This invention relates to novel quinolinyl- and naphthalenylbenzamides or benylamines and related disclosed compounds of the formula ##STR1## wherein X is nitrogen, NO or CR.sup.1 ; Y is C(R.sup.1)(R.sup.2)O, OC(R.sup.1)(R.sup.2), C(R.sup.1)(R.sup.2)N(R.sup.3), N(R.sup.3)C(R.sup.1)(R.sup.2) or C(R.sup.1).dbd.C(R.sup.2); wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen or lower alkyl containing 1 to 10 carbon atoms; Z is oxygen or (R.sup.1)(R.sup.2); R.sup.4 is R.sup.1, benzyl, benzyl ring substituted with R.sup.5, benzyl alpha monosubstituted with R.sup.1, benzyl ring substituted with R.sup.5 and alpha monosubstituted with R.sup.1, phenyl, phenylalkyl containing 2 to 10 carbon atoms in the alkyl group or phenylalkyl ring substituted with R.sup.5 and containing 2 to 10 carbon atoms in the alkyl group; wherein R.sup.5 is R.sup.1, lower alkoxy containing 1 to 10 carbon atoms, halogen, trihalomethyl, NO.sub.2, N(R.sup.1)(R.sup.2) or C(O)N(R.sup.1)(R.sup.2); R.sup.6 is R.sup.1 or R.sup.6 is C(O)(R.Type: GrantFiled: October 3, 1990Date of Patent: May 18, 1993Assignee: American Home Products CorpoorationInventors: John H. Musser, Albert J. Molinari, Dominick Mobilio
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Patent number: 5212303Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents (i) ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --0--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjuctive tissues.Type: GrantFiled: September 28, 1992Date of Patent: May 18, 1993Assignee: Centre International de Recherches Dermatologiques (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 5206242Abstract: Compounds of formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or methyl,A is en ethylene or methylene radical which is unsubstituted or substituted by methyl, hydroxyl or oxo,L is a saturated or unsaturated five-membered or six-membered heterocyclic structure which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.6 -alkyl, or C.sub.1 -C.sub.4 -alkanoyl and has from 1 to 3 heteroatoms from the group consisting of N, O and S, the second and third heteroatoms being a nitrogen atom,R.sup.3 is hydrogen, a hydroxy or C.sub.1 -C.sub.6 -alkoxy group,R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen or methoxy,R.sup.5 is hydrogen or methoxy or tert-butyl,R.sup.6 is hydrogen, methyl, nitrile or a C.sub.2 -C.sub.10 -ketal group or the radical --CHR.sup.7 OR.sup.8 --CHR.sup.7 --NR.sup.9 R.sup.10, --COR.sup.11, --SR.sup.12, ##STR2## in which R.sup.7 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.8 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.Type: GrantFiled: September 3, 1991Date of Patent: April 27, 1993Assignee: BASF AktiengesellschaftInventors: Hans-Heiner Wuest, Bernd Janssen, William V. Murray, Michael P. Wachter, Stanley Bell
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Patent number: 5196532Abstract: Compounds of formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or methyl, A is an ethylene or methylene radical which is unsubstituted or substituted by methyl, hydroxyl or oxo,L is a saturated or unsaturated five-membered or six-membered heterocyclic structure which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.6 -alkyl, or C.sub.1 -C.sub.4 -alkanoyl and has from 1 to 3 heteroatoms from the group consisting of N, O and S, the second and third heteroatoms being a nitrogen atom,R.sup.3 is hydrogen, a hydroxy or C.sub.1 -C.sub.6 -alkoxy group,R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen or methoxy,R.sup.5 is hydrogen or methoxy or tert-butyl,R.sup.6 is hydrogen methyl, nitrile or a C.sub.2 -C.sub.10 -ketal group or the radical --CHR.sup.7 OR.sup.8 --CHR.sup.7 --NR.sup.9 R.sup.10, --COR.sup.11, --SR.sup.12, ##STR2## in which R.sup.7 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.8 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.Type: GrantFiled: June 18, 1991Date of Patent: March 23, 1993Assignee: BASF AktiengesellschaftInventors: Hans-Heiner Wuest, Bernd Janssen, William V. Murray, Michael P. Wachter, Stanley Bell
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Patent number: 5196454Abstract: The invention relates to novel 2,5-diaminotetralines of the formula: ##STR1## wherein R1, R2, R3 and R4 are defined herein, processes for preparing them and their use in pharmaceutical compositions. The novel 2,5-diaminotetralines are useful in treating diseases caused by disorders of the dopaminergic systems.Type: GrantFiled: June 15, 1990Date of Patent: March 23, 1993Assignee: Boehringer Ingelheim KGInventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
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Patent number: 5196439Abstract: A cyclic amine is defined by the formula: ##STR1## in which A is naphthyl, phenyl, quinolyl or alkyl, X is a group containing carbonyl, n is 2 or 3 and B is alkyl, halogen, phenyl or --YZ, Y being --O--, --CO-- or --NH--, Z being phenyl, naphthyl, pyridyl, alkyl or cycloalkyl. It is useful to treat mental symptoms associated with a cerebrovascular disease.Type: GrantFiled: January 24, 1992Date of Patent: March 23, 1993Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Norio Karibe, Isao Saito, Kunizo Higurashi, Masahiro Yonaga, Takeru Kaneko, Takahiro Nakazawa, Masataka Ueno, Kiyomi Yamatsu, Kohshi Ueno, Masuhiro Ikeda
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Patent number: 5189045Abstract: The invention relates to new compounds of formula I: ##STR1## in which: m represents zero, 1, 2, 3 or 4,n and p represent zero, 1 or 2,W represents an oxygen atom, an --NH-- radical, or a single bond,R represents a benzocyclobuten-1-yl radical, or an indanyl radical, a 2,3-dihydrobenzofuran-2-ylR.sub.1 represents a hydrogen atom, an alkyl radical having from 1 to 6 carbon atoms, or an aryl radical, andR.sub.2 represents a hydrogen atom, an alkyl radical, an alkenyl radical, a cycloalkyl radical, a benzyl radical, a phenyl radical, an aralkyl radical, an alkoxyalkyl radical or a polyhalogenated alkyl radical, the optical isomers thereof and the addition salts thereof with a pharmaceutically acceptable organic or mineral acid, and medicaments containing the same.Type: GrantFiled: May 17, 1991Date of Patent: February 23, 1993Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Francis Colpaert
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Patent number: 5183889Abstract: A benzonphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjuctive tissues.Type: GrantFiled: December 9, 1991Date of Patent: February 2, 1993Assignee: Centre International de Recherches Dermatologiques (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 5177069Abstract: The present invention provides a novel class of naphthylsulfonylalkanoic acid compounds such as a structure corrresponding to the formula: ##STR1## or a pharmaceutically acceptable salt thereof. A present invention naphthylsulfonylalkanoic acid compound is useful for prevention or treatment of irritable bowel syndrome, biliary dyskinesia and acute pancreatitis.Type: GrantFiled: December 6, 1990Date of Patent: January 5, 1993Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Makio Kitazawa, Masuo Akahane, Yasushi Nakano, Atsushi Tsubaki, Kazuaki Sato, Masaaki Ban, Michihiro Kobayashi
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Patent number: 5158961Abstract: Novel piperidine compounds having the formula ##STR1## wherein the symbols have the same meaning as set forth in the specification, and salts thereof with a pharmaceutically acceptable acid, are disclosed.The novel compound are useful in the treatment of anoxia, migraine, ischemia and epilepsy.Type: GrantFiled: March 22, 1991Date of Patent: October 27, 1992Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Jorgen Drejer
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Patent number: 5153225Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andx denotes oxygen, sulphur or NR.sup.5,and their salts.Type: GrantFiled: April 9, 1991Date of Patent: October 6, 1992Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 5149359Abstract: The present invention relates to derivatives of 3,4-dehydropiperidin-5-one having herbicidal activity. The derivatives have the formula ##STR1## as defined in the claims. The present invention further relates to a herbicidal composition and a method for controlling weeds which grow among agricultural crops.Type: GrantFiled: February 21, 1990Date of Patent: September 22, 1992Assignee: Agrimont S.p.A.Inventors: Giovanni Camaggi, Giovanni Meazza, Ciro Preziuso
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Patent number: 5149714Abstract: The present invention provides novel aryloxy indanamines of the formula ##STR1## wherein n, p and q are each independently 0, 1 or 2,Y and X are each independently lower alkyl, lower alkoxy, hydroxy, CF.sub.3, halogeno or when p or q are 2 and each of the Y or each of the X groups are on adjacent aryl carbon atoms, both of the X or both of the Y groups can be taken together to form a methylenedioxy moiety,R.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl, aralkyl, or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached are pyrrolidino, morpholino, piperidino, piperazino, or 4-methylpiperazino,or an acid addition salt thereof, which are useful as antidepressants and as inhibitors of synaptic norepinephrine and serotonin uptake.Type: GrantFiled: August 15, 1990Date of Patent: September 22, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Jules Freedman
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Patent number: 5118684Abstract: A novel piperidine derivative is defined by the formula (I), including a slt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.Type: GrantFiled: April 3, 1991Date of Patent: June 2, 1992Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 5110986Abstract: This application relates to a process for preparing a N-t-alkyl-1,2-diacylhydrazine by reacting a 1,3,4-oxadiazole with a tertiary alkyl cation precursor in the presence of a strong acid catalyst. Preferably, the 1,3,4-oxadiazole is a 2,5-disubstituted-1,3,4-oxadiazole and more preferably a 2,5-diaryl-1,3,4-oxadiazole. The strong acid catalyst is preferably a sulfur containing acid and more preferably sulfuric acid.Type: GrantFiled: April 26, 1988Date of Patent: May 5, 1992Assignee: Rohm and Haas CompanyInventor: Martha J. Kelly
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Patent number: 5102911Abstract: HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed.Type: GrantFiled: July 6, 1990Date of Patent: April 7, 1992Assignee: Merck & Co, Inc.Inventors: Ta J. Lee, Wilbur J. Holtz
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Patent number: 5102894Abstract: Novel piperidine compounds having the formula I ##STR1## wherein R.sup.3 is 3,4-methylenedioxyphenyl, phenyl, naphthyl, which are optionally substituted with one or two halogen, amino, C.sub.1-6 -alkyl mono-or disubstituted amino group, C.sub.1-6 -alkoxy, cyano, mono-, di- or trihalogenated C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.1-6 alkyl, C.sub.3-5 -alkylene, trifluoromethoxy, or trifluoromethyl groups,R.sup.1 is hydrogen, straight or branched C.sub.1-8 -alkyl, C.sub.1-8 -alkoxy-C.sub.1-8 -alkyl, C.sub.3-8 -cycloalkyl, C.sub.2-6 -alkenyl, C.sub.4-8 -cycloalkylalkyl, C.sub.2-6 -alkynylZ is hydrogen, straight or branched C.sub.1-8 -alkyl,Y is O or SX is O, S or NR, wherein R is hydrogen or C.sub.1-4 -alkylor a salt thereof with a pharmaceutically acceptable acid.The novel compounds are useful in the treatment of anoxia, traumatic injury, ischemia, migraine and epilepsy.Type: GrantFiled: December 3, 1990Date of Patent: April 7, 1992Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Ursula Sonnewald
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Patent number: 5100901Abstract: A cyclic amine compound is defined by the formula: ##STR1## in which J is indanyl, indanonyl, indenyl, indenonyl, indanedionyl, tetralonyl, benzosuberonyl, indanolyl or a divalent group thereof, K is phenyl, an arylalkyl or cynnamyl, B is --(CHR22) r--, R22 being H or methyl, --CO-- (CHR22)r--, .dbd.(CH--CH.dbd.CH)b--, .dbd.CH--(CH2)c-- or .dbd.(CH--CH)d.dbd. and the ring including T and Q is piperidine. The compound is useful to treat senile dementia.Type: GrantFiled: October 18, 1989Date of Patent: March 31, 1992Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Yutaka Tsuchiya, Kunizou Higurashi, Norio Karibe, Youichi Iimura, Atsushi Sasaki, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Takashi Kosasa, Atsuhiko Kubota, Michiko Kosasa, Kiyomi Yamatsu
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Patent number: 5098931Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) and (II): ##STR1##Type: GrantFiled: September 24, 1990Date of Patent: March 24, 1992Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Wasyl Halczenko, George D. Hartman
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Patent number: 5089507Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom,R.sub.3 is hydrogen, C.sub.1-6 alkyl or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 and R.sub.5 are independently hydrogen, hydroxyl, halogen, C.sub.1-6 alkyl or aryl, provided both R.sub.4 and R.sub.5 are not simultaneously hydrogen; and p is an integer from 1 to 4,is useful for the treatment of pain or hyponatraemic disease states.Type: GrantFiled: September 25, 1989Date of Patent: February 18, 1992Assignee: Dr. L. Zambeletti SpAInventors: Vittorio Vecchietti, Roberto Colle, Antonio Giordani, Giulio Dondio